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353495-21-3

353495-21-3 Structure

353495-21-3 Structure
IdentificationBack Directory
[Name]

3H-Cyclopenta[c]quinoline, 3a,4,5,9b-tetrahydro-8-nitro-4-phenyl-
[CAS]

353495-21-3
[Synonyms]

BAP1-IN-1
3H-Cyclopenta[c]quinoline, 3a,4,5,9b-tetrahydro-8-nitro-4-phenyl-
[Molecular Formula]

C18H16N2O2
[MOL File]

353495-21-3.mol
[Molecular Weight]

292.33
Chemical PropertiesBack Directory
[Boiling point ]

454.3±45.0 °C(Predicted)
[density ]

1.239±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

0.26±0.40(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].
[in vivo]

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice[1].

Animal Model:NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model[1]
Dosage:50 mg/kg/d
Administration:Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:Significantly delayed progression of disease in both models.
[References]

[1] Wang L, et al. Epigenetic targeted therapy of stabilized BAP1 in ASXL1 gain-of-function mutated leukemia. Nat Cancer. 2021 May;2(5):515-526. DOI:10.1038/s43018-021-00199-4
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